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辅料和加工条件对消旋卡多曲结晶共附聚形成团聚体的影响。

Influence of excipients and processing conditions on the development of agglomerates of racecadotril by crystallo-co-agglomeration.

作者信息

Garala Kevin, Patel Jaydeep, Patel Anjali, Raval Mihir, Dharamsi Abhay

机构信息

Department of Pharmaceutics, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot, Gujarat, India.

出版信息

Int J Pharm Investig. 2012 Oct;2(4):189-200. doi: 10.4103/2230-973X.106996.

DOI:10.4103/2230-973X.106996
PMID:23580935
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3618635/
Abstract

PURPOSE

The purpose of the present investigation was to improve the flow and mechanical properties of racecadotril by a crystallo-co-agglomeration (CCA) technique. Direct tableting is a requirement of pharmaceutical industries. Poor mechanical properties of crystalline drug particles require wet granulation which is uneconomical, laborious, and tedious.

MATERIALS AND METHODS

The objective of this work was to study the influence of various polymers/excipients and processing conditions on the formation of directly compressible agglomerates of the water-insoluble drug, racecadotril, an antidiarrheal agent. The agglomerates of racecadotril were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for racecadotril as well as a bridging liquid for the agglomeration of the crystallized drug and water as the nonsolvent. The prepared agglomerates were tested for micromeritic and mechanical properties.

RESULTS

The process yielded ~90 to 96% wt/ wt spherical agglomerates containing racecadotril with the diameter between 299 and 521 μ. A higher rotational speed of crystallization system reduces the size of the agglomerates and disturbs the sphericity. Spherical agglomerates were generated with a uniform dispersion of the crystallized drug. CCA showed excellent flowability and crushing strength.

CONCLUSION

Excipients and processing conditions can play a key role in preparing spherical agglomerates of racecadotril by CCA, an excellent alternative to the wet granulation process to prepare intermediates for direct compression.

摘要

目的

本研究的目的是通过结晶共附聚（CCA）技术改善消旋卡多曲的流动性和机械性能。直接压片是制药行业的一项要求。结晶药物颗粒较差的机械性能需要湿法制粒，而湿法制粒既不经济，又费力且繁琐。

材料与方法

本研究的目的是研究各种聚合物/辅料以及加工条件对水不溶性药物消旋卡多曲（一种止泻剂）直接压片附聚物形成的影响。消旋卡多曲的附聚物采用二氯甲烷（DCM）-水作为结晶体系制备。DCM既是消旋卡多曲的良溶剂，也是结晶药物附聚的架桥液，水作为非溶剂。对制备的附聚物进行了粉体学和机械性能测试。

结果

该工艺得到了约90%至96%（重量/重量）的含消旋卡多曲的球形附聚物，直径在299至521μm之间。结晶体系较高的转速会减小附聚物的尺寸并扰乱球形度。生成的球形附聚物中结晶药物分散均匀。CCA显示出优异的流动性和抗压强度。

结论

辅料和加工条件在通过CCA制备消旋卡多曲球形附聚物中起着关键作用，CCA是湿法制粒工艺的一种极佳替代方法，可用于制备直接压片的中间体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/4f3472c55e62/IJPI-2-189-g029.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/35cb73b7c9f0/IJPI-2-189-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/e22180837721/IJPI-2-189-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/df2f67cd43b4/IJPI-2-189-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/d46dab395b24/IJPI-2-189-g018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/0ed108b30c89/IJPI-2-189-g019.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/88186d8381fa/IJPI-2-189-g024.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/c6434dd65fd6/IJPI-2-189-g025.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/e908b5ab3ae1/IJPI-2-189-g027.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/4f3472c55e62/IJPI-2-189-g029.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/35cb73b7c9f0/IJPI-2-189-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/e22180837721/IJPI-2-189-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/df2f67cd43b4/IJPI-2-189-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/d46dab395b24/IJPI-2-189-g018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/0ed108b30c89/IJPI-2-189-g019.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/88186d8381fa/IJPI-2-189-g024.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/c6434dd65fd6/IJPI-2-189-g025.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/e908b5ab3ae1/IJPI-2-189-g027.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb69/3618635/4f3472c55e62/IJPI-2-189-g029.jpg

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